Abdalhameed Manahil M, Zhao Pingwei, Hurst Dow P, Reggio Patricia H, Abood Mary E, Croatt Mitchell P
Department of Chemistry and Biochemistry, Natural Products and Drug Discovery Center, University of North Carolina at Greensboro, Greensboro, NC 27402, United States.
Department of Anatomy and Cell Biology and Center for Substance Abuse Research, Temple University, Philadelphia, PA 19140, United States.
Bioorg Med Chem Lett. 2017 Feb 1;27(3):612-615. doi: 10.1016/j.bmcl.2016.12.012. Epub 2016 Dec 5.
The first structure-activity relationships for a benzothiazole scaffold acting as an antagonist at GPR35 is presented. Analogues were designed based on a lead compound that was previously determined to have selective activity as a GPR35 antagonist. The synthetic route was modular in nature to independently explore the role of the middle and both ends of the scaffold. The activities of the analogues illustrate the importance of all three segments of the compound.
首次报道了作为GPR35拮抗剂的苯并噻唑支架的构效关系。基于先前确定具有作为GPR35拮抗剂的选择性活性的先导化合物设计了类似物。合成路线本质上是模块化的，以独立探索支架中间部分和两端的作用。类似物的活性说明了化合物所有三个部分的重要性。
